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CAS No.: 638156-11-3

CID 2011756 Catalog No. CSN15791

Synonyms: CID-2011756

CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells.

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400-920-2911

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描述Protein kinase D (PKD) is a novel family of serine/threonine kinases regulated by diacylglycerol, which is involved in multiple cellular processes and various pathological conditions^[2]. CID 2011756 is an ATP competitive PKD inhibitor, with an IC₅₀ of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC₅₀, 0.6 and 0.7 µM, respectively)^[2]. Confirmed in vitro PKD1 inhibitors are then evaluated for their ability to inhibit the phosphorylation of endogenously expressed PKD1 ser⁹¹⁶, an indicator of cellular PKD1 kinase activity. Results shows that CID 2011756 inhibites the phosphorylation of Ser⁹¹⁶-PKD1 at levels greater than 50%. CID 2011756 is the most potent of the inhibitors with a cellular EC₅₀ of 10 ± 0.7 µM (n = 3). Moreover, we counter screened 2011756 in IMAP-based CDK7, AKT and PLK1 assays, and find no kinase inhibition at concentrations up to 50 µM^[2]. Moreover, preliminary in vitro data suggests that our most potent cell active PKD1 inhibitor, CID 2011756, has pan-PKD inhibitory effects (pKD2 IC₅₀ = 0.6 ± 0.1; pKD3 IC₅₀ = 0.7 ± 0.2 µM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor^[2].
参考文献

[1] Sharlow ER, Mustata Wilson G, et al. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.
[2] Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134. doi: 10.1371/journal.pone.0025134. Epub 2011 Oct 5. PMID: 21998636; PMCID: PMC3187749.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5197 mL
- 12.5987 mL
- 25.1974 mL
- 5 mM
- 0.5039 mL
- 2.5197 mL
- 5.0395 mL
- 10 mM
- 0.2520 mL
- 1.2599 mL
- 2.5197 mL

技术信息

CAS号

638156-11-3

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H21ClN2O3

运输

蓝冰

分子量

396.87

别名

CID-2011756

溶解度

DMSO	113.0 mg/mL (284.7 mM)
Water	insoluble

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